Aurora Kinase Suppliers USA

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Aurora Kinase A active human, Recombinant Aurora A kinase also known as serine/threonine-protein kinase 6 is an enzyme that in humans is encoded by the AURKA gene. Aurora A is a member of a family of mitotic serine/threonine kinases. It is implicated with important processes during mitosis and meiosis whose proper function is integral for healthy cell proliferation. Aurora A is activated by one or more phosphorylations and its activity peaks during the G2 phase to M phase transition in the cell cycle. Human aurora kinase a (genbank accession no. nm_003600), amino acids 2-403 with n-terminal his6-tag, mw=50 kda, expressed in a baculovirus infected sf9 cell expression system. Applications: Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling. Group: Enzymes. Synonyms: Aurora Kinase A; Aurora A kinase; serine/threonine-protein kinase 6; AURKA; AIK; ARK1; AURA; AURORA2; BTAK; PPP1R47; STK15; STK6; STK7. Purity: > 90% (SDS-PAGE). ARK1. Mole weight: mol wt 50 kDa. Activity: ~17,000 units/mg protein. Form: aqueous solution. Source: baculovirus infected Sf9 cells. Species: Human. Aurora Kinase A; Aurora A kinase; serine/threonine-protein kinase 6; AURKA; AIK; ARK1; AURA; AURORA2; BTAK; PPP1R47; STK15; STK6; STK7. Pack: Minimum 50 ng protein/vial by Bradford. Cat No: NATE-0087. Creative Enzymes
Aurora kinase inhibitor-2 Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC 50 s of 310 nM and 240 nM for Aurora A and Aurora B , respectively [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 331770-21-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112355. MedChemExpress MCE
Aurora Kinase Inhibitor II The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. Aurora kinase inhibitor II is a cell-permeable anilinoquinazoline that blocks the activity of Aurora A with IC50 of 0.39 μM. This compound has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. This compound has the ability to permeate the cell and is involved in the regulation of the cell cycle, particularly cell division. Synonyms: 4-(4?-Benzamidoanilino)-6,7-dimethoxyquinazoline. Grades: ≥98%. CAS No. 331770-21-9. Molecular formula: C23H20N4O3. Mole weight: 400.4. BOC Sciences
Aurora Kinase Inhibitor III Aurora kinase inhibitor III is a potent ATP-competitive aurora related kinase inhibitor with IC50 of 42 nM. Aurora kinase inhibitor III is a cell-permeable, 2,4-dianilinopyrimidine compound which has been used to study a variety of tumor types. It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR (IC50s = 386, 3,550, 591, 1,980, 2,510, 887, and >10,000 nM, respectively). Aurora kinase protein levels are elevated in c-myc-driven B-cell lymphomas in both mice and humans. Study of the inhibition of Aurora kinase proteins could lead to potential treatments for malignancies. Synonyms: Aurora Kinase Inhibitor III; AKI-7169; AKI 7169; AKI7169. Grades: ≥98%. CAS No. 879127-16-9. Molecular formula: C21H18F3N5O. Mole weight: 413.4. BOC Sciences
Aurora Kinase Inhibitor VI, ZM447439 (4-(4-(N-Benzoylamino)anilino)-6- methoxy-7- (3- (1-morpholino) propoxy) quinazoline) A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50=110 and 130nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50=0.88, 1.03 and 1.79uM for Lck, Src and MEK1, respectively, and IC50>10uM for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20uM, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 331771-20-1. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 4
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Aurora 3, Control peptide (STK13, Serine Threonine Kinase 13, Aurora C, AIE2, AIK3, Aurora Related Kinase 3, Aurora/IPL1-like) A synthetic peptide derived from the N-terminus of the human Aurora-3 protein. Group: Molecular Biology. Grades: Purified. Pack Sizes: 100ug. US Biological Life Sciences. USBiological 1
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PF 03814735 (Aurora Kinases A and B, N-[2-[(1S,4R)-6-[[4-(Cyclobutylamin o)-5-(trifluoromethyl)-2-pyrimidinyl]amino]-1,2,3, 4-tetrahydronaphthalen-1,4-imin-9-yl]-2-oxoethyl]- acetamide) ATP-competitive inhibitor of Aurora kinases A and B (IC50 values are 0.8 and 5nm for recombinant Aurora B and Aurora A, respectively). Inhibits phosphorylation of Aurora B, histone H3 and Aurora A in cultured MDA-MB-231 cells (IC50 values are ~20, 50 and 150nm respectively). Shown to block cytokinesis; inhibits cellular proliferation in several human tumor cell lines, including HCT-116, HL-60, A549 and H125, and in human xenograft mouse models. Orally available. Group: Biochemicals. Grades: Highly Purified. CAS No. 942487-16-3. Pack Sizes: 10mg. US Biological Life Sciences. USBiological 3
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1-(3-Chloropropoxy)-4-fluorobenzene 1-(3-Chloropropoxy)-4-fluorobenzene was used as a reagent in the preparation of a library of hydantoin compds which has used to study Aurora kinase A inhibitory activity. It was also used as an alkylation agent in the preparation of tetracyclic quinoxaline butyrophenones as 5-HT2A and postsynaptic D2 antagonists and inhibitors of serotonin transporter for treatment of neuropsychiatric and neurological disorders. Group: Biochemicals. Grades: Highly Purified. CAS No. 1716-42-3. Pack Sizes: 1g, 5g. Molecular Formula: C9H10ClFO, Molecular Weight: 188.63. US Biological Life Sciences. USBiological 9
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1,3-Cycloheptanedione 1,3-Cycloheptanedione is an intermediate used to prepare pyrrole-indolin-2-ones as aurora kinase inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 1194-18-9. Pack Sizes: 500mg, 1g. Molecular Formula: C7H10O2, Molecular Weight: 126.15. US Biological Life Sciences. USBiological 9
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2,5-Difluorobenzyl Bromide 2,5-Difluorobenzyl Bromide is used as a reagent in the synthesis of phthalazinone pyrazoles as potent inhibitors of Aurora-A kinase. Also used as a reagent in the synthesis of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase. Group: Biochemicals. Grades: Highly Purified. CAS No. 85117-99-3. Pack Sizes: 1g, 10 g. Molecular Formula: C7H5BrF2, Molecular Weight: 207.02. US Biological Life Sciences. USBiological 10
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2-Amino-5-thiazoleacetic Acid Ethyl Ester 2-Amino-5-thiazoleacetic Acid Ethyl Ester is an intermediate used to synthesize thiazoloquinazoline derivatives as potent selective aurora A and B kinase inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 62557-32-8. Pack Sizes: 100mg, 1g. Molecular Formula: C7H10N2O2S, Molecular Weight: 186.23. US Biological Life Sciences. USBiological 9
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7-Fluoro-4(3H)-quinazolinone 7-Fluoro-4(3H)-quinazolinone is a fluorinated quinazolin-4(3H)-one with poly(ADP-ribose)polymerase-1 (PARP-1) inhibitory activity. 7-Fluoro-4(3H)-quinazolinone is also used as an intermediate in the preparation of the aurora kinase inhibitor AZD1152. Group: Biochemicals. Alternative Names: 7-Fluoro-3,4-dihydroquinazolin-4-one; 7-Fluoro-3H-quinazolin-4-one; 7-Fluoroquinazolin-4(3H)-one; 7-Fluoroquinazolin-4-ol. Grades: Highly Purified. CAS No. 16499-57-3. Pack Sizes: 1g. US Biological Life Sciences. USBiological 2
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AKI-001 AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Synonyms: AKI-001; AKI 001; AKI001. Grades:>98%. CAS No. 925218-37-7. Molecular formula: C21H24N4O. Mole weight: 348.45. BOC Sciences 2
AKI603 AKI603 is an inhibitor of Aurora kinase A (AurA) with IC50 of 12.3 nM. It can induce senescence in chronic myeloid leukemia cells carrying the T315I mutation. AKI603 shows strong anti-proliferative activity in leukemia cells. Synonyms: AKI-603. Grades: 98%. CAS No. 1432515-73-5. Molecular formula: C19H23N9O2. Mole weight: 409.4. BOC Sciences
Alisertib Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor ( IC 50 =1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: MLN 8237. CAS No. 1028486-01-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg; 500 mg. Product ID: HY-10971. MedChemExpress MCE
Alisertib MLN8237 is a second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Aurora kinase inhibitor MLN8237 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Synonyms: MLN8237; MLN-8237; MLN 8237; alisertib. Benzoic acid, 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-. Grades: 0.98. CAS No. 1028486-01-2. Molecular formula: C27H20ClFN4O4. Mole weight: 518.9. BOC Sciences
AMG 900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC 50 of 5 nM, 4 nM and 1 nM for Aurora A , B and C , respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 945595-80-2. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13253. MedChemExpress MCE
AMG-900 AMG 900 is a small-molecule inhibitor of Aurora kinases A, B and C with potential antineoplastic activity. Aurora kinase inhibitor AMG 900 selectively binds to and inhibits the activities of Aurora kinases A, B and C, which may result in inhibition of cellular division and proliferation in tumor cells that overexpress these kinases. Synonyms: AMG900; AMG-900; AMG 900. Grades: 0.98. CAS No. 945595-80-2. Molecular formula: C28H21N7OS. Mole weight: 503.57764. BOC Sciences
Anti-Cancer Active Compound Library A unique collection of 2114 compounds with known anti-cancer activity for high throughput screening (HTS) and high content screening (HCS); - Effective tool for molecular mechanism of tumorigenesis, and anti-tumor drug screening; - Covers various major targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc. - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2160. Categories: Anti-Cancer Active Compounds Libraries. TARGETMOL CHEMICALS
Anti-Cancer Approved Drug Library A unique collection of 1726 approved anti-cancer drugs for high throughput screening (HTS) and high content screening (HCS); - These FDA, EMA, or NMPA approved anti-cancer drugs have annotated bioactivity, safety, and bioavailability; - Effective tool for cancer research and drug repurposing screening; - Covers various major targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc. , in lung cancer, breast cancer, leukemia, lymphoma, etc. - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2110. Categories: Anti-Cancer Approved Drug Libraries. TARGETMOL CHEMICALS
Anti-Cancer Clinical Compound Library A unique collection of 1990 anti-cancer compounds for high throughput screening (HTS) and high content screening (HCS); - Bioactivity confirmed by pre-clinical research and all of them are currently in clinical trial phases, representing the cutting-edge treatments for cancers; - Effective tool for cancer research and drug repurposing screening; - Covers various major targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc. , in lung cancer, breast cancer, leukemia, lymphoma, etc. - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2120. Categories: Anti-Cancer Clinical Compounds Libraries. TARGETMOL CHEMICALS
Anti-Cancer Compound Library A unique collection of 5885 compounds with anti-cancer activity for high throughput screening (HTS) and high content screening (HCS); - Bioactivity and safety profiled in (confirmed by) pre-clinical and clinical settings (research and trials); - Effective tool for molecular mechanism of tumorigenesis, and anti-tumor drug screening; - Covers various major targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc. - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2100. Categories: Anti-Cancer Compounds Libraries. TARGETMOL CHEMICALS
Anti-Cancer Drug Library A unique collection of 2478 anticancer drugs for high throughput screening (HTS) and high content screening (HCS); - Bioactivity and safety profiled in (confirmed by) pre-clinical and clinical settings (research and trials), an effective tool for molecular mechanism of tumorigenesis, and anti-tumor drug repositioning drug discovery; - Covers various major targets including PI3K, HDAC, mTOR, CDK, Aurora Kinase, JAK, etc; involved in 15 different cancer research areas, such as lung cancer, breast cancer, leukemia, lymphoma, etc. - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L2150. Categories: Anti-Cancer Drug Libraries. TARGETMOL CHEMICALS
At9283 AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo. Group: Inhibitors. Alternative Names: 1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)urea;1-Cyclopropyl-3-(3-(5-(morpholinomethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)ureaAT9283;AT9283, >=98%;N-cyclopropyl-N-[3-[5-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]Urea;Urea, N-cyclopropyl-N-[3-[6-(4-morpholinylmethyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl]-. CAS No. 896466-04-9. Molecular formula: C19H23N7O2. Mole weight: 381.438. Purity: 0.997. Density: 1.45. Catalog: ACM896466049. Alfa Chemistry.
AT9283 AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC50= 3, 3, 1.2, 1.1, and 4 nM, respectively). It also potently (IC50 = <1 μM) inhibits serine/threonine kinases as well as receptor and non-receptor tyrosine kinases. Synonyms: AT9283; AT 9283; AT-9283. Grades: >98%. CAS No. 896466-04-9. Molecular formula: C19H23N7O2. Mole weight: 381.43. BOC Sciences
AT9283 AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B , JAK2/3 , Abl (T315I) and Flt3 ( IC 50 s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 896466-04-9. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-50514. MedChemExpress MCE
AT-9283 L-lactate AT9283 is a multikinase inhibitor, is also a small-molecule inhibitor of several kinases with potential antineoplastic activity. AT9283 binds to and inhibits Aurora kinases A and B, JAK2 (Janus kinase 2) and the kinase BCR-ABL, which may result in the inhibition of cellular division and proliferation and the induction of apoptosis in tumor cells that overexpress these kinases. Synonyms: AT 9283; AT9283. CAS No. 896466-76-5. Molecular formula: C19H23N7O2. Mole weight: 471.52. BOC Sciences 2
Aurora A inhibitor II Aurora A inhibitor II is a potent and selective inhibitor of Aurora A kinase (AurA; IC50 = 4.3 nM). Synonyms: 4-[[2-[[4-[2-(4-acetyl-1-piperazinyl)-2-oxoethyl]phenyl]amino]-5-fluoro-4-pyrimidinyl]amino]-N-(2-chlorophenyl)-Benzamide. Grades: 99%. CAS No. 1158838-43-7. Molecular formula: C31H29ClFN7O3. Mole weight: 602.06. BOC Sciences
Autophagy Compound Library A unique collection of 1248 compounds with defined autophagy-inducing or -inhibitory activity for research in autophagy, high throughput screening (HTS) and high content screening (HCS) for new drugs; - Bioactivity and safety confirmed by pre-clinical research and clinical trials; - Targets include Autophagy inducers, Autophagy inhibitors, Proteasome, HIF, HDAC, Aurora Kinase, E3 Ligase, mTOR, etc; - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC validated to ensure high purity and quality. Uses: Scientific use. Product Category: L3200. Categories: Autophagy Compounds Libraries. TARGETMOL CHEMICALS
AZD1152, TFA Salt An Aurora kinase inhibitor, used to treat patients with advanced solid tumors. Group: Biochemicals. Alternative Names: 3-[[7-[3-[Ethyl[2- (phosphonooxy) ethyl]amino]propoxy]-4-quinazolinyl]amino]-N- (3-fluorophenyl) -1H-pyrazole-5-acetamide Trifluoroacetic Acid Salt; Barasertib Trifluoroacetic Acid Salt; AZD-1152 Trifluoroacetic Acid Salt. Grades: Highly Purified. CAS No. 957881-03-7. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C??H??FN?O?P; x(C ?HF?O?), Molecular Weight: 587.54. US Biological Life Sciences. USBiological 6
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Barasertib Barasertib is an orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152-hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Synonyms: AZD1152; AZD-1152; AZD 1152; Barasertib. CAS No. 722543-31-9. Molecular formula: C26H31FN7O6P. Mole weight: 587.54. BOC Sciences 10
BI-847325 BI-847325 is an orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Group: Inhibitors. Alternative Names: BI-847325; BI 847325; BI847325. CAS No. 1207293-36-4. Molecular formula: C29H28N4O2. Mole weight: 464.57. Appearance: Solid powder. Purity: >98%. IUPACName: (Z)-3- (3- ( (4- ( (dimethylamino)methyl)phenylamino) (phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide. Canonical SMILES: O=C (NCC)C#CC1=CC (NC/2=O)=C (C=C1)C2=C (NC3=CC=C (CN (C)C)C=C3)/C4=CC=CC=C4. Catalog: ACM1207293364-1. Alfa Chemistry.
BI-847325 BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Synonyms: BI-847325; BI 847325; BI847325. Grades: 98%. CAS No. 1207293-36-4. Molecular formula: C29H28N4O2. Mole weight: 464.56. BOC Sciences 8
Binucleine 2 Binucleine 2 is an inhibitor of cytokinesis function of the ARK-2 pathway. It is also an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki = 0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. Synonyms: Binucleine 2; 220088-42-6; N'-[2-(3-chloro-4-fluorophenyl)-4-cyanopyrazol-3-yl]-N,N-dimethylmethanimidamide; N'-(1-(3-Chloro-4-fluorophenyl)-4-cyano-1H-pyrazol-5-yl)-N,N-dimethyliminoformamide; HMS546I06; Probes1_000319; Probes2_000073; CHEMBL1598812; DTXSID90430554; Binucleine 2, >=97% (HPLC); CCG-41865; MFCD00177827; AKOS040755467; NCGC00165742-01; J-014418; SR-01000631912-1; N'-(1-(3-Chloro-4-fluorophenyl)-4-cyano-1H-pyrazol-5-yl)-N,N-dimethylformimidamide. Grades: ≥98%. CAS No. 220088-42-6. Molecular formula: C13H11ClFN5. Mole weight: 291.7. BOC Sciences 10
BPR1K653 SBPR1K653 is a potent Aurora kinase inhibitor with potential anticancder activity. BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats., BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments. Synonyms: BPR1K653; BPR1K 653; BPR1K-653. Grades: 98%. CAS No. 1192754-07-6. Molecular formula: C30H30Cl2N6O2. Mole weight: 541.04. BOC Sciences 11
CCT129202 CCT129202 is an inhibitor of Aurora kinase activity and displays a favorable antineoplastic effect in preclinical studies. CCT129202 significantly reversed ABCB1- and ABCG2-mediated MDR in vitro, in vivo and ex vivo by inhibiting the function of their transporters and enhanced the eradication of cancer stem-like cells by chemotherapeutic agents. CCT129202 may be a candidate as MDR reversal agent for antineoplastic combination therapy and merits further clinical investigation. Synonyms: CCT129202; CCT-129202; CCT 129202. CAS No. 942947-93-5. Molecular formula: C23H25ClN8OS. Mole weight: 497.02. BOC Sciences 10
CCT-137690 CCT137690, an aurora kinase inhibitor CCT137690, is a highly selective, orally bioavailable imidazo[4,5-b]pyridine derivative that inhibits Aurora A and B kinases with low nanomolar IC50 values in both biochemical and cellular assays and exhibits anti-proliferative activity against a wide range of human solid tumour cell lines. CCT137690 efficiently inhibits histone H3 and TACC3 phosphorylation (Aurora B and Aurora A substrates, respectively) in HCT116 and HeLa cells. Continuous exposure of tumour cells to the inhibitor causes multipolar spindle formation, chromosome misalignment, polyploidy and apoptosis. This is accompanied by p53/p21/BAX induction, thymidine kinase 1 (TK1) downregulation and PARP cleavage. Furthermore, CCT137690 treatment of MYCN-amplified neuroblastoma cell lines inhibits cell proliferation and decreases MYCN protein expression. Importantly, in a transgenic mouse model of neuroblastoma (TH-MYCN) that overexpresses MYCN protein and is predisposed to spontaneous neuroblastoma formation, this compound significantly inhibits tumour growth. The potent preclinical activity of CCT137690 suggests that this inhibitor may benefit patients with MYCN amplified neuroblastoma. Synonyms: CCT-137690. CCT 137690. CCT137690. CAS No. 1095382-05-0. Molecular formula: C26H31BrN8O. Mole weight: 551.48. BOC Sciences 10
CD532 CD532 is a potent Aurora A kinase inhibitor with an IC 50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1639009-81-6. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-112273. MedChemExpress MCE
CD532 hydrochloride CD532 hydrochloride is a potent Aurora A kinase inhibitor with an IC 50 of 45 nM. CD532 hydrochloride has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 hydrochloride also can directly interact with AURKA and induces a global conformational shift. CD532 hydrochloride can be used for the research of cancer [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2926498-81-7. Pack Sizes: 5 mg; 10 mg; 25 mg. Product ID: HY-112273A. MedChemExpress MCE
Cell Cycle Compound Library A unique collection of 695 cell cycle related compounds for high throughput screening (HTS) and high content screening (HCS); - Targets include CDK, ROCK, Aurora Kinase, ATM/ATR, DNA-PK, DNA/RNA Synthesis, etc. ; - Effective tool for research in cell cycle and related diseases, such as cancer, cardiovascular diseases, inflammation, neurodegenerative diseases, etc. ; - Detailed compound information with structure, target, activity, IC50 value, and biological activity description; - Structurally diverse, medicinally active, and cell permeable; - NMR and HPLC/LCMS validated to ensure high purity and quality. Uses: Scientific use. Product Category: L8100. Categories: Cell Cycle Compounds Libraries. TARGETMOL CHEMICALS
Chiauranib Chiauranib (CS2164) is an orally active multi-target inhibitor against tumor angiogenesis. Chiauranib potently inhibits the angiogenesis-related kinases ( VEGFR1 , VEGFR2 , VEGFR3 , PDGFRα and c-Kit ), mitosis-related kinase Aurora B , and chronic inflammation-related kinase CSF-1R , with IC 50 values ranging from 1-9 nM. Chiauranib has strongly anticancer effects [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Ibcasertib; CS2164. CAS No. 1256349-48-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-124526. MedChemExpress MCE
CYC116 CYC116 is an orally bioavailable small molecule multi-kinase inhibitor with antineoplastic activity. Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis. Aurora kinases are serine/threonine protein kinases that are only expressed in actively dividing cells and are critical in division or mitosis. VEGFR2 is a receptor tyrosine kinase that appears to account for most of the mitogenic and chemotactic effects of vascular endothelial growth factor (VEGF) on adult endothelial cells. Group: Inhibitors. Alternative Names: CYC116; CYC 116; CYC-116. CAS No. 693228-63-6. Molecular formula: C18H20N6OS. Mole weight: 368.46. Appearance: Solid powder. Purity: >98%. IUPACName: 4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine. Canonical SMILES: NC1=NC (C)=C (C2=NC (NC3=CC=C (N4CCOCC4)C=C3)=NC=C2)S1. Catalog: ACM693228636. Alfa Chemistry.
CYC-116 An Aurora kinase inhibitor, used to treat patients with advanced solid tumors. Group: Biochemicals. Alternative Names: 5-[2, 5-Dihydro-2-[[4- (4-morpholinyl) phenyl]imino]-4-pyrimidinyl]-4-methyl-2-thiazolamine. Grades: Highly Purified. CAS No. 1059105-22-4. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 2
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Danusertib An Aurora kinase inhibitor, used to treat patients with chromic myeloid leukemia. Group: Biochemicals. Alternative Names: 4- (4-Methyl-1-piperazinyl) -N- [1, 4, 5, 6-tetrahydro-5- [ (2R) -2-methoxy-2-phenylacetyl]pyrrolo [3, 4-c]pyrazol-3-yl]benzamide; PHA 739358. Grades: Highly Purified. CAS No. 827318-97-8. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 2
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Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed. This agent may preferentially bind to and inhibit Aurora B kinase. Aurora kinases, a family of serine-threonine kinases, are important regulators of cellular proliferation and division. Synonyms: PHA739358; PHA-739358; PHA 739358; Danusertib. CAS No. 827318-97-8. Molecular formula: C26H30N6O3. Mole weight: 474.55. BOC Sciences 10
Derrone Derrone, a prenylated isoflavones, is an Aurora kinase inhibitor, with IC50 values of 6 and 22.3 μM against Aurora B and Aurora A, respectively. Derrone shows anti-tumor activity. Group: Inhibitors. CAS No. 76166-59-1. Molecular formula: C20H16O5. Mole weight: 336.34. Canonical SMILES: O=C1C2=C (O)C=C3C (C=CC (C) (C)O3)=C2OC=C1C4=CC=C (O)C=C4. Catalog: ACM76166591. Alfa Chemistry.
ENMD-2076 ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has been shown to inhibit a distinct profile of angiogenic tyrosine kinase targets in addition to the Aurora A kinase. Aurora kinases are key regulators of mitosis (cell division), and are often over-expressed in human cancers. ENMD-2076 also targets the VEGFR, Flt-3 and FGFR3 kinases which have been shown to play important roles in the pathology of several cancers. ENMD-2076 has shown promising activity in Phase 1 clinical trials in solid tumor cancers, leukemia, and multiple myeloma. ENMD-2076 is currently in a Phase 2 trial for ovarian cancer, and preclinical and clinical activities are ongoing in assessing the compound's applicability for other forms of cancer. Synonyms: ENMD-2076; ENMD 2076; ENMD2076. CAS No. 934353-76-1. Molecular formula: C21H25N7. Mole weight: 375.47. BOC Sciences 8
ERK Inhibitor VIII ((S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide) A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2nM against Erk2; [ATP] = 65uM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4uM; IC50 ≥1uM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100nM WZ4002 with or without 1uM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 896720-20-0. Pack Sizes: 10mg. Molecular Formula: C??H??Cl?FN?O?. US Biological Life Sciences. USBiological 4
Worldwide
Focal Adhesion Kinase Inhibitor III (FAK Inhibitor III, N-(4-tert-Butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine-4,4-dioxide) A cell-permeable pyrazolobenzothiazined ioxide compound that targets and locks FAK in its inactive conformation, resulting in preincubation time-dependent inhibition in kinase assays and FAK autophosphorylation in human prostate cancer PC3M-luc cells (IC50 = 7.1uM with 30 min inhibitor preincubation), while exhibiting little activity toward Akt1, Aurora B, HER2, MEK1, p38alpha, Pyk2, or Src even at concentrations as high as 10uM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences. USBiological 4
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Glycyl-H 1152 dihydrochloride Glycyl-H 1152 dihydrochloride is a glycyl analog of the Rho-kinase inhibitor H 1152 dihydrochloride with an improved selectivity for ROCKII (IC50 = 0.0118, 2.35, 2.57, 3.26, > 10 and >10 μM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC, respectively). Glycyl-H 1152 dihydrochloride is used for the treatment of hypertension and arteriosclerosis. Uses: The treatment of hypertension and arteriosclerosis. Synonyms: (S)-(+)-4-Glycyl-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride; 2-amino-1-[(3S)-3-methyl-4-(4-methylisoquinolin-5-yl)sulfonyl-1,4-diazepan-1-yl]ethanone dihydrochloride. Grades: ≥99% by HPLC. CAS No. 913844-45-8. Molecular formula: C18H24N4O3S.2HCl. Mole weight: 449.4. BOC Sciences 10
GSK-1070916A GSK-1070916A is an ATP-competitive inhibitor of the serine/threonine kinases Aurora B and C with potential antineoplastic activity. Aurora B/C kinase inhibitor GSK1070916A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types. Synonyms: GSK 1070916; GSK-1070916; GSK 1070916; GSK1070916A; GSK-1070916A; GSK 1070916A; NMI-900; NMI 900; NMI900. CAS No. 942918-07-2. Molecular formula: C30H33N7O. Mole weight: 507.63. BOC Sciences 10
GSK 2250665A GSK 2250665A is an Itk inhibitor (pKi = 9.2) displaying selectivity for Itk over Aurora B kinase and Btk (pIC50 = 6.4 and 6.5, respectively) and a panel of other kinases. GSK 2250665A was shown to inhibit IFNγ production in PBMCs. Synonyms: GSK-2250665A; GSK 2250665A; GSK2250665A; GSK-2250665; GSK 2250665; GSK2250665; trans-4-[[4-[(6-Ethyl-2-benzothiazolyl)amino]-6-(phenylmethyl)-2-pyrimidinyl]amino]cyclohexanol. Grades: ≥97% by HPLC. CAS No. 1246030-96-5. Molecular formula: C26H29N5OS. Mole weight: 459.61. BOC Sciences 10
HATU HATU, a triazolopyridine dirivative, has been found to be a peptide coupling reagent and could be used in the formation of of Aurora A kinase inhibitors. Synonyms: HATU; 2-(7-Aza-1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; O-(7-Azabenzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate; 1H-1,2,3-Triazolo[4,5-b]pyridinium, 1-[bis(dimethylamino)methylene]-, 3-oxide, hexafluorophosphate(1-) (1:1); O-(7-Azabenzotriazol-1-yl)-N,N,N,N-tetramethyl uronium hexafluorophosphate; 1H-1,2,3-Triazolo[4,5-b]pyridinium, 1-[bis(dimethylamino)methylene]-, hexafluorophosphate(1-), 3-oxide; 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate. Grades: 98%. CAS No. 148893-10-1. Molecular formula: C10H15F6N6OP. Mole weight: 380.23. BOC Sciences 3
Hesperadin Hesperadin is an inhibitor of human Aurora B, which can prevent the phosphorylation of substrate with IC(50) of 40 nM. Growth of cultured bloodstream forms was also sensitive to Hesperadin (IC(50) of 50 nM). Hesperadin blocked nuclear division and cytokinesis but not other aspects of the cell cycle. Consequently, growth arrested cells accumulated multiple kinetoplasts, flagella and nucleoli, similar to the effects of RNAi-dependent knockdown of TbAUK1 in cultured bloodstream forms cells. Molecular models predicted high-affinity binding of Hesperadin to both conserved and novel sites in TbAUK1. Collectively, these data demonstrate that cell cycle progression is essential for infections with T. brucei and that parasite Aurora kinases can be targeted with small-molecule inhibitors. Synonyms: Hesperadin. Grades: ≥98% (HPLC). CAS No. 422513-13-1. Molecular formula: C29H32N4O3S. Mole weight: 516.65. BOC Sciences 10
IKK epsilon/TBK1 Inhibitor II, MRT67307 (TANK Binding Kinase 1/IKKinducible Inhibitor II, N- (3- (5-Cyclopropyl -2- (3- (morpholino methyl ) phenylamino) pyrimidin-4-ylamino) propyl ) cyclobutane carboxamide) A cell-permeable BX795 analog that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKK epsilon (IC50 = 19 and 160nM, respectively) with excellent selectivity over IKKalpha and IKKbeta (IC50 > 10uM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC50 = 27, 52, 36, and 41nM, respectively), SIK2 (IC50 = 67nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1uM) in a 108-kinase panel. Increases TNF-alpha-stimulated NF-kB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflammÂ… Group: Biochemicals. Grades: Highly Purified. CAS No. 495-85-2. Pack Sizes: 5mg. Molecular Formula: C??H??N?O?. US Biological Life Sciences. USBiological 4
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Ilorasertib Ilorasertib, also know as ABT-348, is a novel, potent and orally bioavailable inhibitor of the Aurora kinases as well as the VEGF and PDGF families of receptor tyrosine kinases and is currently in Phase I clinical trials. ABT-348 has nanomolar potency (IC50) for inhibiting binding and cellular auto-phosphorylation of Aurora B (7 and 13 nM), C (1 and 13 nM) and A (120 and 189 nM). These results provide the rationale for clinical assessment of ABT-348 as a therapeutic agent in the treatment of cancer. Uses: Antineoplastic agents. Synonyms: ABT-348; Abbott 968660. Grades: 0.98. CAS No. 1227939-82-3. Molecular formula: C25H21FN6O2S. Mole weight: 488.541. BOC Sciences 10
INH-13 INH-13 is an Aurora Kinase inhibitor. Synonyms: INH 13; INH13; Benzamide, N-[5-[[7-[(2S)-2-hydroxy-3-(1-piperidinyl)propoxy]-6-methoxy-4-quinazolinyl]amino]-2-pyrimidinyl]-. Grades: 98%. CAS No. 1016971-82-6. Molecular formula: C28H31N7O4. Mole weight: 529.59. BOC Sciences 11
JAB-2485 JAB-2485 is a potent and selective Aurora kinase A (AURKA) inhibitor, with an IC 50 of 0.33 nM. JAB-2485 exhibits around 1700-fold selectivity for AURKA over AURKB. JAB-2485 induces cell cycle arrest and apoptosis. JAB-2485 can be used for the research of cancer [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2899209-55-1. Pack Sizes: 1 mg; 5 mg; 10 mg; 25 mg. Product ID: HY-157396. MedChemExpress MCE
Jadomycin B Jadomycin B is an angucyclic natural product produced by Streptomyces venezuelae ISP5230. It exhibits antimicrobial, antitumor activity and inhibits aurora-B kinase and DNA cleaving. It was also shown to be effective against a variety of staphylococci. Synonyms: 1-(sec-butyl)-12-((4,5-dihydroxy-6-methyltetrahydro-2H-pyran-2-yl)oxy)-7-hydroxy-5-methyl-8H-benzo[b]oxazolo[3,2-f]phenanthridine-2,8,13(1H,3aH)-trione; 8H-Benzo(b)oxazolo(3,2-f)phenanthridine-2,8,13(1H,3aH)-trione, 12-((2,6-dideoxyhexopyranosyl)oxy)-7-hydroxy-5-methyl-1-(1-methylpropyl)-. Grades: ≥98% by HPLC. CAS No. 149633-99-8. Molecular formula: C30H31NO9. Mole weight: 549.6. BOC Sciences 5
JH295 JH295 is an irreversible, cysteine-targeted inhibitor of the human centrosomal kinase, Nek2. JH295 irreversibly inhibited cellular Nek2 without affecting the mitotic kinases, Cdk1, Aurora B, or Plk1. Moreover, JH295 did not perturb bipolar spindle assembly or the spindle assembly checkpoint. To our knowledge, JH295 is the first small molecule shown to inactivate Nek2 kinase activity in cells. Synonyms: JH 295; JH-295; 3-[(2-Ethyl-4-methyl-1H-imidazole)-5-ylmethylene]-5-[(1-oxo-2-propynyl)amino]-1H-indole-2(3H)-one. CAS No. 1311143-71-1. Molecular formula: C18H16N4O2. Mole weight: 320.35. BOC Sciences 11
JNJ-7706621 JNJ-7706621 is a novel cell cycle inhibitor that showed potent inhibition of several cyclin-dependent kinases (CDK) and Aurora kinases and selectively blocked proliferation of tumor cells of various origins but was about 10-fold less effective at inhibiting normal human cell growth in vitro. In human cancer cells, treatment with JNJ-7706621 inhibited cell growth independent of p53, retinoblastoma, or P-glycoprotein status; activated apoptosis; and reduced colony formation. At low concentrations, JNJ-7706621 slowed the growth of cells and at higher concentrations induced cytotoxicity. Synonyms: JNJ-7706621; JNJ-7706621; JNJ-7706621. CAS No. 443797-96-4. Molecular formula: C15H12F2N6O3S. Mole weight: 394.36. BOC Sciences 10
JNJ-7706621 JNJ-770662 is a broad spectrum inhibitor of cyclin-dependent kinases and aurora kinases including CDK1/Cyclin B, CDK2/Cyclin A, CDK2/Cyclin E, Aurora-A and Aurora-B. JNJ-770662 has been shown to induce growth suppression and mitotic defects, these results suggest that JNJ-7706621 could be useful for cell cycle analysis and therapy of various cancers, including Ewing's sarcoma. Group: Biochemicals. Alternative Names: N3-[4-(Aminosulfonyl)phenyl]-1-(2,6-difluorobenzoyl)-1H-1,2,4-triazole-3,5-diamine; 4- [ [5-Amino-1- (2, 6-difluorobenzoyl) -1H- [1, 2, 4] triazol-3-yl] amino] benzenesulfonamide; JNJ 770662. Grades: Highly Purified. CAS No. 443797-96-4. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 2
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Kw-2449 KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively. Group: Inhibitors. CAS No. 1000669-72-6. Molecular formula: C20H20N4O. Mole weight: 332.4. Purity: >99%. Catalog: ACM1000669726. Alfa Chemistry.
LDC1267 LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8. Synonyms: LDC1267; LDC 1267; LDC-1267. Grades: >98%. CAS No. 1361030-48-9. Molecular formula: C30H26F2N4O5. Mole weight: 560.55. BOC Sciences 8
LY3295668 LY3295668 (AK-01) is a potent, orally active and highly specific Aurora-A kinase inhibitor, with K i values of 0.8 nM and 1038 nM for AurA and AurB, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AK-01. CAS No. 1919888-06-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-114258. MedChemExpress MCE
MK-5198 MK-5108 is a novel small molecule with potent inhibitory activity against Aurora-A kinase. Although most of the Aurora-kinase inhibitors target both Aurora-A and Aurora-B, MK-5108 specifically inhibited Aurora-A kinase in a panel of protein kinase assays. Inhibition of Aurora-A by MK-5108 in cultured cells induced cell cycle arrest at the G(2)-M phase in flow cytometry analysis. The effect was confirmed by the accumulation of cells with expression of phosphorylated Histone H3 and inhibition of Aurora-A autophosphorylation by immunostaining assays. MK-5108 also induced phosphorylated Histone H3 in skin and xenograft tumor tissues in a nude rat xenograft model. MK-5108 inhibited growth of human tumor cell lines in culture and in different xenograft models. Furthermore, the combination of MK-5108 and docetaxel showed enhanced antitumor activities compared with control and docetaxel alone-treated animals without exacerbating the adverse effects of docetaxel. MK-5108 is currently tested in clinical trials and offers a new therapeutic approach to combat human cancers as a single agent or in combination with existing taxane therapies. Synonyms: MK5108; MK-5108; MK 5108; VX689; VX 689; VX-689. Grades: >98%. CAS No. 1010085-13-8. Molecular formula: C22H21ClFN3O3S. Mole weight: 461.94. BOC Sciences 10
MLN8054 MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers. Synonyms: MLN8054; MLN 8054; MLN-8054. CAS No. 869363-13-3. Molecular formula: C25H15ClF2N4O2. Mole weight: 476.86. BOC Sciences 10
MLN8054 MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC 50 of 4 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 869363-13-3. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10180. MedChemExpress MCE
MLN 8054 An Aurora kinase inhibitor, used to treat patients with advanced solid tumors. Group: Biochemicals. Alternative Names: 4-[[9-Chloro-7-(2,6-difluorophenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]benzoic Acid. Grades: Highly Purified. CAS No. 869363-13-3. Pack Sizes: 5mg. US Biological Life Sciences. USBiological 2
Worldwide
MLN 8237 Antagonist of Aurora A serine/threonine protein kinase; antineoplastic. Group: Biochemicals. Alternative Names: 4-[[9-Chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxy-benzoic acid; Alisertib. Grades: Highly Purified. CAS No. 1028486-01-2. Pack Sizes: 10mg. Molecular Formula: C27H20ClFN4O4, Molecular Weight: 518.92. US Biological Life Sciences. USBiological 7
Worldwide

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